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Physicochemical properties

 

Aqueous solubility

The solubility of a compound is an important factor in determining its absorption from the gastrointestinal tract and ultimately its oral bioavailability. Poor solubility can also limit the quality of the data generated in other in vitro assays.

Cyprotex provide both a turbidimetric solubility service and a thermodynamic solubility service for measurement of aqueous solubility. The contrasting features of these methods are described in our online ADME guide.

 

Lipophilicity

Lipophilicity is a key determinant of the pharmacokinetic behaviour of drugs. It can influence distribution into tissues, absorption and the binding characteristics of a drug, as well as being an important factor in determining the solubility of a compound.

Cyprotex provide a log P (partition coefficient) service using Sirius GLpKa technology,a log D shake flask service (octanol/buffer) and a HPLC based Chomatographic Hydrophobicity Index (CHI) service for determining lipophilicity.

 

pKa determination

The pKa of a molecule predicts the degree of ionisation the molecule will have at a particular pH. The ionisation potential of a compound affects the distribution of the chemical in solution and affects the availability of the chemical to enter into physical, chemical and biological reactions. The pKa of a compound influences properties such as logD and solubility as well as the absorption, distribution, metabolism, elimination and potency of a compound.

Cyprotex provide a pKa and log P determination assay using a potentiometric titration method (GLpKa) technology developed by Sirius.

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8th north america drug discovery workshop
ADMET for Medicinal Chemists: A Practical Guide
ADMET for Medicinal Chemists: A Practical Guide
By Dr. Katya Tsaioun, Chief Scientific Officer, Cyprotex
Wiley & Sons, March 2011
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This website was last updated
on 3rd February 2012
This website is intended to assist investors, industry participants, customers and employees to understand Cyprotex’s global operations and ambitions.
Certain information and detail is disclosed in the interest of compliance of AIM Rule 26.